摘要 |
3-Hydroxypyridin-4-one derivs. of formula (I) their stereoisomers, tautomers and salts are new: R1 = H, halo, alkyl, alkoxy, alkoxycarbonyl, NH2, alkylamino, dialkylamino, aminocarbonyl, N-alkylaminocarbonyl, N,N-dialkylaminocarbonyl, COOH, alkylsulphonyl, aminosulphonyl, CN, OH, NO2, tetrazolyl, or alkylenedioxy (which, together with B, forms an oxygen-contg. heterocyclic ring); R2 = H, alkyl, alkylenehydroxy, alkylenealkoxy, alkylenecarboxy, alkylcarbonyl-alkoxy, alkylenamine, N-alkanoyalkylenamine, alkanoyloxyalkylene, formylalkylene, or, together with either A or R3, forms an oxygen-contg. heterocyclic ring; R3 = H, alkyl, COOH, alkanoyloxylalkylene, aminocarbonyl, N-alkylaminocarbonyl or N,N-dialkylaminocarbonyl; R4 = H, alkanoyl, alkoxycarbonyl or a residue which is fissionable under physiological conditions; A = opt. substd. methylene or carbamyl; B = aryl or heteroaryl. All carbon-chains are 'lower' and may be substd.. Aryl, heteroaryl and oxygen-contg. heterocycles may also be substd. |